JP2007314551A5 - - Google Patents
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- Publication number
- JP2007314551A5 JP2007314551A5 JP2007182287A JP2007182287A JP2007314551A5 JP 2007314551 A5 JP2007314551 A5 JP 2007314551A5 JP 2007182287 A JP2007182287 A JP 2007182287A JP 2007182287 A JP2007182287 A JP 2007182287A JP 2007314551 A5 JP2007314551 A5 JP 2007314551A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- phenyl
- cycloalkyl
- substituted
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims 398
- -1 cyano, thio Chemical group 0.000 claims 225
- 125000000753 cycloalkyl group Chemical group 0.000 claims 168
- 150000001875 compounds Chemical class 0.000 claims 142
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 140
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 138
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 131
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 127
- 125000001072 heteroaryl group Chemical group 0.000 claims 124
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 119
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 116
- 125000005842 heteroatom Chemical group 0.000 claims 104
- 125000003118 aryl group Chemical group 0.000 claims 86
- 125000003545 alkoxy group Chemical group 0.000 claims 77
- 125000004104 aryloxy group Chemical group 0.000 claims 77
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 77
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 61
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 60
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 claims 60
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 59
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 59
- 125000003710 aryl alkyl group Chemical group 0.000 claims 50
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 50
- 125000005843 halogen group Chemical group 0.000 claims 43
- 229910052757 nitrogen Inorganic materials 0.000 claims 35
- 125000004093 cyano group Chemical group *C#N 0.000 claims 29
- 238000000034 method Methods 0.000 claims 26
- 125000004429 atom Chemical group 0.000 claims 24
- 125000003342 alkenyl group Chemical group 0.000 claims 23
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 23
- 125000000304 alkynyl group Chemical group 0.000 claims 23
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 23
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 23
- 125000005143 heteroarylsulfonyl group Chemical group 0.000 claims 23
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 20
- 125000001424 substituent group Chemical group 0.000 claims 20
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 19
- 238000000926 separation method Methods 0.000 claims 19
- 125000005647 linker group Chemical group 0.000 claims 18
- 229910052760 oxygen Inorganic materials 0.000 claims 13
- 229910052717 sulfur Inorganic materials 0.000 claims 13
- 125000001475 halogen functional group Chemical group 0.000 claims 12
- 239000003814 drug Substances 0.000 claims 9
- 238000004519 manufacturing process Methods 0.000 claims 9
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 8
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 8
- ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Chemical compound O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 claims 8
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 8
- 239000001301 oxygen Substances 0.000 claims 8
- 239000011593 sulfur Substances 0.000 claims 8
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Substances N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 claims 7
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims 6
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Chemical group C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 6
- 239000008196 pharmacological composition Substances 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 150000003335 secondary amines Chemical group 0.000 claims 5
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 4
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000006504 o-cyanobenzyl group Chemical group [H]C1=C([H])C(C#N)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 4
- 150000003512 tertiary amines Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 229910052794 bromium Inorganic materials 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- XSCHRSMBECNVNS-UHFFFAOYSA-N quinoxaline Chemical group N1=CC=NC2=CC=CC=C21 XSCHRSMBECNVNS-UHFFFAOYSA-N 0.000 claims 3
- JASGBRKRMPRRTD-UHFFFAOYSA-N 2-[(6-chloro-2,4-dioxopyrimidin-1-yl)methyl]benzonitrile Chemical compound ClC1=CC(=O)NC(=O)N1CC1=CC=CC=C1C#N JASGBRKRMPRRTD-UHFFFAOYSA-N 0.000 claims 2
- BVUJISIVAHYNLI-UHFFFAOYSA-N 2-[(6-chloro-3-methyl-2,4-dioxopyrimidin-1-yl)methyl]benzonitrile Chemical compound O=C1N(C)C(=O)C=C(Cl)N1CC1=CC=CC=C1C#N BVUJISIVAHYNLI-UHFFFAOYSA-N 0.000 claims 2
- JTRLDOQRNPDZPC-UHFFFAOYSA-N 2-[[6-(3-aminopiperidin-1-yl)-2,4-dioxo-3-[(3-pyrrol-1-ylphenyl)methyl]pyrimidin-1-yl]methyl]benzonitrile Chemical compound C1C(N)CCCN1C(N(C1=O)CC=2C(=CC=CC=2)C#N)=CC(=O)N1CC1=CC=CC(N2C=CC=C2)=C1 JTRLDOQRNPDZPC-UHFFFAOYSA-N 0.000 claims 2
- KYXUNUKTHMZSLE-UHFFFAOYSA-N 2-[[6-(3-aminopiperidin-1-yl)-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile Chemical compound C1C(N)CCCN1C1=CC(=O)NC(=O)N1CC1=CC=CC=C1C#N KYXUNUKTHMZSLE-UHFFFAOYSA-N 0.000 claims 2
- WKSHWJJTTMKYRY-UHFFFAOYSA-N 2-[[6-(3-aminopiperidin-1-yl)-3-(1h-benzimidazol-2-ylmethyl)-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile Chemical compound C1C(N)CCCN1C(N(C1=O)CC=2C(=CC=CC=2)C#N)=CC(=O)N1CC1=NC2=CC=CC=C2N1 WKSHWJJTTMKYRY-UHFFFAOYSA-N 0.000 claims 2
- KVIRZRAVCGZEMX-UHFFFAOYSA-N 2-[[6-(3-aminopiperidin-1-yl)-3-[(2-cyanophenyl)methyl]-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile Chemical compound C1C(N)CCCN1C(N(C1=O)CC=2C(=CC=CC=2)C#N)=CC(=O)N1CC1=CC=CC=C1C#N KVIRZRAVCGZEMX-UHFFFAOYSA-N 0.000 claims 2
- OYCQUHWGCMEPNI-UHFFFAOYSA-N 2-[[6-(3-aminopiperidin-1-yl)-3-[(4-cyanophenyl)methyl]-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile Chemical compound C1C(N)CCCN1C(N(C1=O)CC=2C(=CC=CC=2)C#N)=CC(=O)N1CC1=CC=C(C#N)C=C1 OYCQUHWGCMEPNI-UHFFFAOYSA-N 0.000 claims 2
- DRSHNENJAZVBLE-UHFFFAOYSA-N 2-[[6-(3-aminopiperidin-1-yl)-5-chloro-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile Chemical compound C=1C=CC=C(C#N)C=1CN1C(=O)N(C)C(=O)C(Cl)=C1N1CCCC(N)C1 DRSHNENJAZVBLE-UHFFFAOYSA-N 0.000 claims 2
- JTRLDOQRNPDZPC-XMMPIXPASA-N 2-[[6-[(3r)-3-aminopiperidin-1-yl]-2,4-dioxo-3-[(3-pyrrol-1-ylphenyl)methyl]pyrimidin-1-yl]methyl]benzonitrile Chemical compound C1[C@H](N)CCCN1C(N(C1=O)CC=2C(=CC=CC=2)C#N)=CC(=O)N1CC1=CC=CC(N2C=CC=C2)=C1 JTRLDOQRNPDZPC-XMMPIXPASA-N 0.000 claims 2
- KYXUNUKTHMZSLE-CQSZACIVSA-N 2-[[6-[(3r)-3-aminopiperidin-1-yl]-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile Chemical compound C1[C@H](N)CCCN1C1=CC(=O)NC(=O)N1CC1=CC=CC=C1C#N KYXUNUKTHMZSLE-CQSZACIVSA-N 0.000 claims 2
- KVIRZRAVCGZEMX-JOCHJYFZSA-N 2-[[6-[(3r)-3-aminopiperidin-1-yl]-3-[(2-cyanophenyl)methyl]-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile Chemical compound C1[C@H](N)CCCN1C(N(C1=O)CC=2C(=CC=CC=2)C#N)=CC(=O)N1CC1=CC=CC=C1C#N KVIRZRAVCGZEMX-JOCHJYFZSA-N 0.000 claims 2
- JJTMVXIGKYTDHI-JOCHJYFZSA-N 2-[[6-[(3r)-3-aminopiperidin-1-yl]-3-[(3-cyanophenyl)methyl]-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile Chemical compound C1[C@H](N)CCCN1C(N(C1=O)CC=2C(=CC=CC=2)C#N)=CC(=O)N1CC1=CC=CC(C#N)=C1 JJTMVXIGKYTDHI-JOCHJYFZSA-N 0.000 claims 2
- OYCQUHWGCMEPNI-JOCHJYFZSA-N 2-[[6-[(3r)-3-aminopiperidin-1-yl]-3-[(4-cyanophenyl)methyl]-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile Chemical compound C1[C@H](N)CCCN1C(N(C1=O)CC=2C(=CC=CC=2)C#N)=CC(=O)N1CC1=CC=C(C#N)C=C1 OYCQUHWGCMEPNI-JOCHJYFZSA-N 0.000 claims 2
- NOKFOTRWCQJAKB-MRXNPFEDSA-N 2-[[6-[(3r)-3-aminopiperidin-1-yl]-3-ethyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile Chemical compound C=1C=CC=C(C#N)C=1CN1C(=O)N(CC)C(=O)C=C1N1CCC[C@@H](N)C1 NOKFOTRWCQJAKB-MRXNPFEDSA-N 0.000 claims 2
- QWCRMWNCTSFODM-CYBMUJFWSA-N 2-[[6-[(3r)-3-aminopiperidin-1-yl]-5-chloro-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile Chemical compound C1[C@H](N)CCCN1C1=C(Cl)C(=O)NC(=O)N1CC1=CC=CC=C1C#N QWCRMWNCTSFODM-CYBMUJFWSA-N 0.000 claims 2
- DRSHNENJAZVBLE-CQSZACIVSA-N 2-[[6-[(3r)-3-aminopiperidin-1-yl]-5-chloro-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile Chemical compound C=1C=CC=C(C#N)C=1CN1C(=O)N(C)C(=O)C(Cl)=C1N1CCC[C@@H](N)C1 DRSHNENJAZVBLE-CQSZACIVSA-N 0.000 claims 2
- UZCQJGIZQLXZPF-UHFFFAOYSA-N 3-[[4-(3-aminopiperidin-1-yl)-3-[(2-cyanophenyl)methyl]-2,6-dioxopyrimidin-1-yl]methyl]benzoic acid Chemical compound C1C(N)CCCN1C(N(C1=O)CC=2C(=CC=CC=2)C#N)=CC(=O)N1CC1=CC=CC(C(O)=O)=C1 UZCQJGIZQLXZPF-UHFFFAOYSA-N 0.000 claims 2
- UZCQJGIZQLXZPF-OAQYLSRUSA-N 3-[[4-[(3r)-3-aminopiperidin-1-yl]-3-[(2-cyanophenyl)methyl]-2,6-dioxopyrimidin-1-yl]methyl]benzoic acid Chemical compound C1[C@H](N)CCCN1C(N(C1=O)CC=2C(=CC=CC=2)C#N)=CC(=O)N1CC1=CC=CC(C(O)=O)=C1 UZCQJGIZQLXZPF-OAQYLSRUSA-N 0.000 claims 2
- IHDDGIBXDUBRFB-UHFFFAOYSA-N 6-(3-aminopiperidin-1-yl)-1,3-bis[(2-bromo-5-fluorophenyl)methyl]pyrimidine-2,4-dione Chemical compound C1C(N)CCCN1C(N(C1=O)CC=2C(=CC=C(F)C=2)Br)=CC(=O)N1CC1=CC(F)=CC=C1Br IHDDGIBXDUBRFB-UHFFFAOYSA-N 0.000 claims 2
- GZBXRROZKDWTHE-UHFFFAOYSA-N 6-(3-aminopiperidin-1-yl)-1-[(2-bromo-5-fluorophenyl)methyl]-3-methylpyrimidine-2,4-dione Chemical compound C=1C(F)=CC=C(Br)C=1CN1C(=O)N(C)C(=O)C=C1N1CCCC(N)C1 GZBXRROZKDWTHE-UHFFFAOYSA-N 0.000 claims 2
- ZOZBXLMDTJHPKM-UHFFFAOYSA-N 6-(3-aminopiperidin-1-yl)-1-[(2-bromophenyl)methyl]-3-methylpyrimidine-2,4-dione Chemical compound C=1C=CC=C(Br)C=1CN1C(=O)N(C)C(=O)C=C1N1CCCC(N)C1 ZOZBXLMDTJHPKM-UHFFFAOYSA-N 0.000 claims 2
- RTNHKNRRDBDENT-UHFFFAOYSA-N 6-(3-aminopiperidin-1-yl)-1-[(2-bromophenyl)methyl]pyrimidine-2,4-dione Chemical compound C1C(N)CCCN1C1=CC(=O)NC(=O)N1CC1=CC=CC=C1Br RTNHKNRRDBDENT-UHFFFAOYSA-N 0.000 claims 2
- MTYQPWCBXKEMEF-UHFFFAOYSA-N 6-(3-aminopiperidin-1-yl)-1-[(2-chloro-4-fluorophenyl)methyl]-3-methylpyrimidine-2,4-dione Chemical compound C=1C=C(F)C=C(Cl)C=1CN1C(=O)N(C)C(=O)C=C1N1CCCC(N)C1 MTYQPWCBXKEMEF-UHFFFAOYSA-N 0.000 claims 2
- SHWTVSFPUGCFIH-UHFFFAOYSA-N 6-(3-aminopiperidin-1-yl)-1-[(2-iodophenyl)methyl]pyrimidine-2,4-dione Chemical compound C1C(N)CCCN1C1=CC(=O)NC(=O)N1CC1=CC=CC=C1I SHWTVSFPUGCFIH-UHFFFAOYSA-N 0.000 claims 2
- SIOPCTQIGVRHCI-CYBMUJFWSA-N 6-[(3r)-3-aminopiperidin-1-yl]-1-[(2,5-dichlorophenyl)methyl]-3-methylpyrimidine-2,4-dione Chemical compound C=1C(Cl)=CC=C(Cl)C=1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1 SIOPCTQIGVRHCI-CYBMUJFWSA-N 0.000 claims 2
- GZBXRROZKDWTHE-CYBMUJFWSA-N 6-[(3r)-3-aminopiperidin-1-yl]-1-[(2-bromo-5-fluorophenyl)methyl]-3-methylpyrimidine-2,4-dione Chemical compound C=1C(F)=CC=C(Br)C=1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1 GZBXRROZKDWTHE-CYBMUJFWSA-N 0.000 claims 2
- ZOZBXLMDTJHPKM-CYBMUJFWSA-N 6-[(3r)-3-aminopiperidin-1-yl]-1-[(2-bromophenyl)methyl]-3-methylpyrimidine-2,4-dione Chemical compound C=1C=CC=C(Br)C=1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1 ZOZBXLMDTJHPKM-CYBMUJFWSA-N 0.000 claims 2
- MTYQPWCBXKEMEF-CYBMUJFWSA-N 6-[(3r)-3-aminopiperidin-1-yl]-1-[(2-chloro-4-fluorophenyl)methyl]-3-methylpyrimidine-2,4-dione Chemical compound C=1C=C(F)C=C(Cl)C=1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1 MTYQPWCBXKEMEF-CYBMUJFWSA-N 0.000 claims 2
- GZBQHUMIMKAYHA-CYBMUJFWSA-N 6-[(3r)-3-aminopiperidin-1-yl]-1-[(2-chloro-5-fluorophenyl)methyl]-3-methylpyrimidine-2,4-dione Chemical compound C=1C(F)=CC=C(Cl)C=1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1 GZBQHUMIMKAYHA-CYBMUJFWSA-N 0.000 claims 2
- SHWTVSFPUGCFIH-GFCCVEGCSA-N 6-[(3r)-3-aminopiperidin-1-yl]-1-[(2-iodophenyl)methyl]pyrimidine-2,4-dione Chemical compound C1[C@H](N)CCCN1C1=CC(=O)NC(=O)N1CC1=CC=CC=C1I SHWTVSFPUGCFIH-GFCCVEGCSA-N 0.000 claims 2
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims 2
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical group C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical group N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 2
- IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical group C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 claims 2
- 150000001602 bicycloalkyls Chemical group 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 150000001732 carboxylic acid derivatives Chemical group 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000003106 haloaryl group Chemical group 0.000 claims 2
- 125000005216 haloheteroaryl group Chemical group 0.000 claims 2
- 229910052740 iodine Inorganic materials 0.000 claims 2
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical group C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 claims 2
- 239000012669 liquid formulation Substances 0.000 claims 2
- LOMSDFFGKJNOEH-UHFFFAOYSA-N methyl 3-[[4-(3-aminopiperidin-1-yl)-3-[(2-cyanophenyl)methyl]-2,6-dioxopyrimidin-1-yl]methyl]benzoate Chemical compound COC(=O)C1=CC=CC(CN2C(N(CC=3C(=CC=CC=3)C#N)C(N3CC(N)CCC3)=CC2=O)=O)=C1 LOMSDFFGKJNOEH-UHFFFAOYSA-N 0.000 claims 2
- LOMSDFFGKJNOEH-JOCHJYFZSA-N methyl 3-[[4-[(3r)-3-aminopiperidin-1-yl]-3-[(2-cyanophenyl)methyl]-2,6-dioxopyrimidin-1-yl]methyl]benzoate Chemical compound COC(=O)C1=CC=CC(CN2C(N(CC=3C(=CC=CC=3)C#N)C(N3C[C@H](N)CCC3)=CC2=O)=O)=C1 LOMSDFFGKJNOEH-JOCHJYFZSA-N 0.000 claims 2
- 239000003791 organic solvent mixture Substances 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- 239000005022 packaging material Substances 0.000 claims 2
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 2
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical group [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 238000000746 purification Methods 0.000 claims 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 2
- 125000006413 ring segment Chemical group 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 229940124530 sulfonamide Drugs 0.000 claims 2
- 229930192474 thiophene Natural products 0.000 claims 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 2
- 238000005406 washing Methods 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- IWYDHOAUDWTVEP-SSDOTTSWSA-N (R)-mandelic acid Chemical compound OC(=O)[C@H](O)C1=CC=CC=C1 IWYDHOAUDWTVEP-SSDOTTSWSA-N 0.000 claims 1
- JYEUMXHLPRZUAT-UHFFFAOYSA-N 1,2,3-triazine Chemical compound C1=CN=NN=C1 JYEUMXHLPRZUAT-UHFFFAOYSA-N 0.000 claims 1
- VMLKTERJLVWEJJ-UHFFFAOYSA-N 1,5-naphthyridine Chemical group C1=CC=NC2=CC=CN=C21 VMLKTERJLVWEJJ-UHFFFAOYSA-N 0.000 claims 1
- FLBAYUMRQUHISI-UHFFFAOYSA-N 1,8-naphthyridine Chemical group N1=CC=CC2=CC=CN=C21 FLBAYUMRQUHISI-UHFFFAOYSA-N 0.000 claims 1
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical group C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims 1
- ATZNEBZXNTYTGK-UHFFFAOYSA-N 2-[[6-(3-aminoazepan-1-yl)-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile Chemical compound C=1C=CC=C(C#N)C=1CN1C(=O)N(C)C(=O)C=C1N1CCCCC(N)C1 ATZNEBZXNTYTGK-UHFFFAOYSA-N 0.000 claims 1
- GMTUWIWFYIFDEX-UHFFFAOYSA-N 2-[[6-(3-aminopiperidin-1-yl)-2,4-dioxo-3-[(4-pyrazol-1-ylphenyl)methyl]pyrimidin-1-yl]methyl]benzonitrile Chemical compound C1C(N)CCCN1C(N(C1=O)CC=2C(=CC=CC=2)C#N)=CC(=O)N1CC1=CC=C(N2N=CC=C2)C=C1 GMTUWIWFYIFDEX-UHFFFAOYSA-N 0.000 claims 1
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| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| US7550590B2 (en) | 2003-03-25 | 2009-06-23 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| WO2005016911A1 (en) * | 2003-08-13 | 2005-02-24 | Takeda Pharmaceutical Company Limited | 4-pyrimidone derivatives and their use as peptidyl peptidase inhibitors |
| JP2007513058A (ja) * | 2003-09-08 | 2007-05-24 | 武田薬品工業株式会社 | ジペプチジルぺプチダーゼ阻害剤 |
| EP1699777B1 (en) | 2003-09-08 | 2012-12-12 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US7501426B2 (en) | 2004-02-18 | 2009-03-10 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions |
| UA85871C2 (uk) | 2004-03-15 | 2009-03-10 | Такеда Фармасьютікал Компані Лімітед | Інгібітори дипептидилпептидази |
| US7931661B2 (en) * | 2004-06-14 | 2011-04-26 | Usgi Medical, Inc. | Apparatus and methods for performing transluminal gastrointestinal procedures |
| DE102004054054A1 (de) | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine |
| JP2008524331A (ja) | 2004-12-21 | 2008-07-10 | 武田薬品工業株式会社 | ジペプチジルペプチダーゼ阻害剤 |
| DE102005035891A1 (de) | 2005-07-30 | 2007-02-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
| PT1931350E (pt) * | 2005-09-14 | 2014-02-12 | Takeda Pharmaceutical | Administração de inibidores de dipeptidil peptidase |
| WO2007033350A1 (en) | 2005-09-14 | 2007-03-22 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors for treating diabetes |
| EP1924567B1 (en) * | 2005-09-16 | 2012-08-22 | Takeda Pharmaceutical Company Limited | Process for the preparation of pyrimidinedione derivatives |
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| GB0526291D0 (en) | 2005-12-23 | 2006-02-01 | Prosidion Ltd | Therapeutic method |
| NZ569661A (en) * | 2005-12-28 | 2011-06-30 | Takeda Pharmaceutical | Therapeutic agent for diabetes |
| ZA200806143B (en) * | 2005-12-28 | 2009-11-25 | Takeda Pharmaceutical | Therapeutic agent for diabetes |
| CN101495464B (zh) * | 2005-12-29 | 2014-03-05 | 詹森药业有限公司 | 激肽原1受体拮抗剂 |
| JP2009531456A (ja) * | 2006-03-28 | 2009-09-03 | 武田薬品工業株式会社 | （ｒ）−３−アミノピペリジン二塩酸塩の調製 |
| PE20071221A1 (es) | 2006-04-11 | 2007-12-14 | Arena Pharm Inc | Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas |
| BRPI0709984A2 (pt) | 2006-04-12 | 2011-08-02 | Probiodrug Ag | inibidores de enzima |
| KR101257378B1 (ko) | 2006-04-19 | 2013-04-23 | 삼진제약주식회사 | 항바이러스성 피리미딘디온 유도체 및 이의 제조 방법 |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| PE20110235A1 (es) | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | Combinaciones farmaceuticas que comprenden linagliptina y metmorfina |
| EA030606B1 (ru) | 2006-05-04 | 2018-08-31 | Бёрингер Ингельхайм Интернациональ Гмбх | Способы приготовления лекарственного средства, содержащего полиморфы |
| TWI394747B (zh) * | 2006-06-23 | 2013-05-01 | Smithkline Beecham Corp | 脯胺醯基羥化酶抑制劑 |
| PT2054040E (pt) * | 2006-08-16 | 2011-06-30 | Novartis Ag | Método para produzir dispersões sólidas de compostos terapêuticos altamente cristalinos |
| UA100497C2 (ru) | 2006-09-07 | 2013-01-10 | Никомед Гмбх | Комбинированное лечение сахарного диабета |
| DK2073810T3 (da) * | 2006-09-13 | 2011-10-31 | Takeda Pharmaceutical | Anvendelse af 2-6-(3-aminio-piperidin-l-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-l-ylmethyl-4-fluor-benzonitril til behandling af diabetes, cancer, autoimmune sygdomme og HIV infektion |
| US8324383B2 (en) | 2006-09-13 | 2012-12-04 | Takeda Pharmaceutical Company Limited | Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile |
| JP5379692B2 (ja) | 2006-11-09 | 2013-12-25 | プロビオドルグ エージー | 潰瘍、癌及び他の疾患の治療のためのグルタミニルシクラーゼの阻害薬としての３−ヒドロキシ−１，５−ジヒドロ−ピロール−２−オン誘導体 |
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| SI2091948T1 (sl) | 2006-11-30 | 2012-07-31 | Probiodrug Ag | Novi inhibitorji glutaminil ciklaze |
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- 2004-12-15 UA UAA200610844A patent/UA85871C2/uk unknown
- 2004-12-15 WO PCT/US2004/042209 patent/WO2005095381A1/en not_active Ceased
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- 2004-12-15 CN CN201110006939.5A patent/CN102134231B/zh not_active Expired - Lifetime
- 2004-12-15 CN CN2011100052676A patent/CN102127053A/zh active Pending
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